Abstract：
:In an attempt to explain the triamterene stone diathesis, we studied the excretion and solubility of triamterene, 1, and its metabolite, the sulfate ester of the hydroxy derivative of triamterene, 3. The urinary excretion pattern and metabolism in stone formers was the same as in other chronic users of triamterene or healthy volunteers. The solubility of triamterene in urine was approximately one-half of its solubility in buffer solution, whereas the sulfate ester, 3, was nearly twice as soluble in urine as in the buffer solution. In the majority of the subjects studied, we found concentrations of 3 which approached or exceeded apparent solubility limits in urine. This was not true for triamterene where most measured urine concentrations were less than the apparent solubility as determined by equilibration. Alteration in the metabolism of triamterene is probably not a causative factor for triamterene nephrolithiasis. The saturation of urine with triamterene and especially with the sulfate ester, 3, may be related to stone formation, but other physical factors play a role in determining the relative amounts of drug found in calculus material.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Sörgel F,Ettinger B,Benet LZdoi
10.1002/jps.2600750205subject
Has Abstractpub_date
1986-02-01 00:00:00pages
129-32issue
2eissn
0022-3549issn
1520-6017pii
S0022-3549(15)47035-2journal_volume
75pub_type
杂志文章abstract：:Acitretin, a retinoid for the treatment of severe psoriasis, exhibits extremely low aqueous solubility and high photosensitivity. This study investigated the effects of the complexation of acitretin with the respective hydroxypropyl-beta-cyclodextrin (HPBCD) and randomly substituted methyl-beta-cyclodextrin (RMBCD) on...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10495
更新日期：2003-12-01 00:00:00
abstract：:Phenytoin-loaded alkyd nanoemulsions were prepared spontaneously using the phase inversion method from a mixture of novel biosourced alkyds and Tween 80 surfactant. Exposure of human adult keratinocytes (HaCaT cells) for 48 h to alkyd nanoemulsions producing phenytoin concentrations of 3.125-200 μg/mL resulted in rela...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2016.06.028
更新日期：2017-01-01 00:00:00
abstract：:Therapeutic antibodies and antibody derivatives comprise the majority of today's biotherapeutics. Routine methods to generate novel antibodies, such as immunization and phage-display, often give rise to several candidates with desired functional properties. On the contrary, resource-intense steps such as the developme...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1002/jps.24430
更新日期：2015-06-01 00:00:00
abstract：:A previous report detailed the derivation and validation of an equation for calculating the Gibbs free energy of liquid-solid adsorption via high-performance liquid chromatography (HPLC). This study utilizes an improved form of that equation in conjunction with an in vitro model of solute adsorption to give an ordered...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600770609
更新日期：1988-06-01 00:00:00
abstract：:This study was designed to assess the effects of cooling rate, storage temperature, and formulation composition on trehalose phase distribution and protein stability in frozen solutions. The data demonstrate that faster cooling rates (>100°C/min) result in trehalose crystallization and protein aggregation as determine...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24646
更新日期：2015-12-01 00:00:00
abstract：:The rapid hydrolysis of epoprostenol to 6-keto-prostaglandin F1 alpha is hydronium ion-catalyzed even at pH 10 or higher. In the presence of 1.0% hexadecyltrimethylammonium chloride, the rate was reduced significantly (1580-fold at pH 2 and 283-fold at a physiological pH). This decrease in the hydrolysis rate is attri...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600710420
更新日期：1982-04-01 00:00:00
abstract：:17-Chloroacetylajmaline and 17-acetylajmaline are reported to have in vivo antiarrhythmic activity and are metabolized by hydrolysis. Since the hydrolysis product, ajmaline, may be the actual antiarrhythmic agent, the hydrolysis of these derivatives by various tissues of the guinea pig, rat, and mouse was determined i...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600640933
更新日期：1975-09-01 00:00:00
abstract：:Coralyne analogues, isomers, and related alkaloids were examined as inhibitors of reverse transcriptase of RNA tumor viruses in the presence of polyriboadenylic acid-oligodeoxythymidylic acid (Poly rA.oligo dT), polydeoxyadenylic acid-oligodeoxythymidylic acid (Poly dA.oligo dT), polyribocytidylic acid-oligodeoxyguany...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600740819
更新日期：1985-08-01 00:00:00
abstract：:Sucrose fatty acid esters are increasingly used as excipients in pharmaceutical products, but few data are available on their toxicity profile, mode of action, and efficacy on intestinal epithelial models. Three water-soluble sucrose esters, palmitate (P-1695), myristate (M-1695), laurate (D-1216), and two reference a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24085
更新日期：2014-10-01 00:00:00
abstract：:The thermodynamic relationship between FI and FII of ethyl 4-aminobenzoate (benzocaine) has been investigated. Slurry conversion experiments show that the transition temperature below which FI is stable is located between 302 K-303 K (29 °C-30 °C). The polymorphs FI and FII have been characterised by infrared spectros...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.07.022
更新日期：2020-11-01 00:00:00
abstract：:The synthesis of diazoketone analogs of amino acids and associated problems were investigated with N-phthaloyl-DL-alanine serving as a model. The carboxyl was activated by conversion to the acid chloride or, under mild conditions, to the mixed anhydride obtained with ethyl chloroformate or dicyclohexylcarbodiimide; th...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670518
更新日期：1978-05-01 00:00:00
abstract：:Human insulin exists in different association states, from monomer to hexamer, depending on the conditions. In the presence of zinc the "normal" state is a hexamer. The structural properties of 20 variants of human insulin were studied by near-UV circular dichroism, fluorescence spectroscopy, and small-angle X-ray sca...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10355
更新日期：2003-04-01 00:00:00
abstract：:The metabolic disposition of 14C-labeled carprofen [(+/-)-6-chloro-alpha-methylcarbazole-2-acetic acid] was investigated in rats, dogs, and humans. Carprofen is eliminated predominantly by biotransformation in these three species. In dogs and rats, the direct conjugation of carprofen to form an ester glucuronide and o...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600691104
更新日期：1980-11-01 00:00:00
abstract：:Aliphatic polyesters have great utility as temporary prosthetics and surgical aids, and in drug delivery systems. Knowledge of the mechanism and pathways of hydrolysis can form a basis for the design and selection of a controlled-release system. Because of the importance of hydrolysis to the properties of such a syste...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600800815
更新日期：1991-08-01 00:00:00
abstract：:A sensitive high-performance liquid chromatographic (HPLC) assay for N-acetylcysteine in human plasma and urine has been developed. The method employs a prechromatographic stage to produce the dinitrophenyl derivative of N-acetylcysteine, which is chromatographed on a 5-microns C18 bonded reverse-phase column using an...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600730736
更新日期：1984-07-01 00:00:00
abstract：:The purpose of this work is to evaluate biodegradable drug carriers with defined size, hydrophobicity, and surface charge density for preferential lymphatic uptake and retention for sustained regional drug delivery. PLGA-PMA:PLA-PEG (PP) nanoparticles of defined size and relative hydrophobicity were prepared by nanopr...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21970
更新日期：2010-04-01 00:00:00
abstract：:To determine how structural changes in antibodies are connected with aggregation, the structural areas of an antibody prone to and/or impacted by aggregation must be identified. In this work, the higher-order structure and biophysical properties of two different monoclonal antibody (mAb) monomers were compared with th...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23754
更新日期：2013-12-01 00:00:00
abstract：:A sensitive, specific, high-performance liquid chromatographic procedure was developed for the measurement of plasma tiflamizole levels. Acidic plasma samples were extracted with three volumes of ether. The ether extracts were combined and evaporated to dryness. The residue was dissolved in acetonitrile, washed with h...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600731245
更新日期：1984-12-01 00:00:00
abstract：:The development of order during the aging of aluminum hydroxide gel prepared by the reaction of aluminum chloride and ammonium hydroxide to a final pH of 7.0 can be monitored by differential thermal analysis. The loss fo acid reactivity upon aging is accompanied by an increase in the temperature and intensity of the d...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600650931
更新日期：1976-09-01 00:00:00
abstract：:Though there is an advantage in using the higher solubility amorphous state in cases where low solubility limits absorption, physical instability poses a significant barrier limiting its use in solid oral dosage forms. Unlike chemical instability, where useful accelerated stability testing protocols are common, no met...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1002/jps.21138
更新日期：2008-04-01 00:00:00
abstract：:The wettability of the (001), (100), and (011) crystallographic facets of macroscopic aspirin crystals has been experimentally investigated using a sessile drop contact angle (theta) method. theta for a nonpolar liquid was very similar for all three facets, though significant theta differences were observed for three ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20841
更新日期：2007-08-01 00:00:00
abstract：:Carboxy group-terminated synthetic polymers--branched poly(ethylene glycol), poly(acryloylmorpholine), and poly(vinylpyrrolidone)--were made amphiphilic by derivatization with phosphatidyl ethanolamine via the terminal carboxy group and then incorporated into lecithin-cholesterol liposomes prepared by the detergent di...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600840904
更新日期：1995-09-01 00:00:00
abstract：:The absorption-enhancing effects of polyamidoamine (PAMAM) dendrimers with various generations (G0-G3) and concentrations [0.1%-1.0% (w/v)] on the pulmonary absorption of peptide and protein drugs were studied in rats. Insulin and calcitonin were chosen as models of peptide and protein drugs, and their pulmonary absor...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22428
更新日期：2011-05-01 00:00:00
abstract：:In liver microsomes, selexipag (NS-304; ACT-293987) mainly undergoes hydrolytic removal of the sulfonamide moiety by carboxylesterase 1 (CES1) to yield the pharmacologically active metabolite MRE-269 (ACT-333679). However, it is not known how much CES in the liver and intestine contributes to the hydrolysis of selexip...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2018.09.022
更新日期：2019-02-01 00:00:00
abstract：:It is demonstrated that the fluid-phase thermodynamics theory conductor-like screening model for real solvents (COSMO-RS) as implemented in the COSMOtherm software can be used for accurate and efficient screening of coformers for active pharmaceutical ingredient (API) cocrystallization. The excess enthalpy, H(ex) , be...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23227
更新日期：2012-10-01 00:00:00
abstract：:It is understood that a potential issue for drugs with poor aqueous solubility is low oral absorption. If oral exposure issues arise when working with a low solubility drug candidate, the common action is to rely on enabling formulations to solve the issue. However, this approach becomes troublesome in the pre-clinica...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2016.04.003
更新日期：2016-06-01 00:00:00
abstract：:Biopharmaceuticals represent an important and growing class of medicines. Immunogenic responses to biopharmaceuticals in patients can sometimes result in reduced safety and efficacy. Although multiple factors are known to influence immunogenicity, our understanding of the complex underlying mechanisms remains imperfec...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23247
更新日期：2012-10-01 00:00:00
abstract：:Regular insulin, NPH insulin, glargine insulin, calcitonin, and human growth hormone were administered to rats nasally with 0.125% tetradecyl-beta-D-maltoside (TDM), or at various times after TDM treatment. Absorption of all five peptides was enhanced initially and diminished in a time-dependent manner as the interval...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21977
更新日期：2010-04-01 00:00:00
abstract：:A multichannel continuous-flow apparatus for dissolution rate measurements is described. Typical data are presented to demonstrate its utility for studies with bulk drug powders as well as with tablets and capsules without any change of setup. Procedures are given for the preparation of powder samples for dissolution ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600641024
更新日期：1975-10-01 00:00:00
abstract：:A procedure for the determination of mianserin, desmethylmianserin, and 8-hydroxymianserin in plasma at therapeutic concentrations by liquid chromatography with electrochemical detection is described. Following a multiple-step extraction from alkaline plasma into methyl-tert-butyl ether, the reconstituted extract was ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600710812
更新日期：1982-08-01 00:00:00
